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Eg5 is a key protein involved in the formation of bipolar spindles. K858 is a selective ATP-uncompetitive mitotic kinesin Eg5 inhibitor. The compound induces mitotic arrest, caspase-3 activation and cell growth inhibition in HCT116 cells.
| Molecular Weight | 277.34 |
| Formula | C13H15N3O2S |
| CAS Number | 72926-24-0 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Kinesin Products |
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| AZ82
AZ82 is a selective kinesin-like protein KIFC1 (HSET/KIFC1) inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1. |
| CW069
CW069 is an allosteric inhibitor of HSET with IC50 of 75 μM, it showed marked activity against HSET in vitro. |
| ARQ 621
ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. |
| EMD534085
EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM. |
| BAY 1217389
BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM. |
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